1. Immunology/Inflammation Protein Tyrosine Kinase/RTK
  2. TREM receptor Syk
  3. T2M-010

T2M-010 is a potent, brain-penetrant TREM2 agonist (Kd = 0.83 μM). T2M-010 activates receptor-proximal signaling, inducing SYK phosphorylation in TREM2-expressing cells, and promotes microglial phagocytosis. T2M-010 can be used for the study of protective microglial responses relevant to Alzheimer’s disease (AD).

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T2M-010

T2M-010 Chemical Structure

CAS No. : 364611-21-2

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Description

T2M-010 is a potent, brain-penetrant TREM2 agonist (Kd = 0.83 μM). T2M-010 activates receptor-proximal signaling, inducing SYK phosphorylation in TREM2-expressing cells, and promotes microglial phagocytosis. T2M-010 can be used for the study of protective microglial responses relevant to Alzheimer’s disease (AD)[1].

In Vitro

T2M010 (25 µM, 1 h) leads to a robust twofold increase in SYK phosphorylation in HEK–hTREM2/DAP12 cells[1].
T2M-010 (25 µM, 30 min) significantly enhances bead uptake in BV2 cells, demonstrating a marked increase in phagocytic activity[1]. T2M-010 shows no cytotoxicity in human fibroblasts (WI-38 and HS-27; IC50 >100 µM), low hERG risk (IC50 > 60 µM), and minimal inhibition of major CYP isoforms at 10 µM (≤ 11.2%)[1].
T2M-010 can return robust A→B transport in MDCK– MDR1 assays (Papp = 2.85 × 10⁻⁵ cm/s) and a low efflux ratio (ER = 1.07), pointing to minimal P-gp–mediated efflux[1].
T2M-010 displays good gastrointestinal stability (> 88-86% parent remaining after 2 h in simulated gastric and intestinal fluids, respectively) and long plasma half-lives (167 min in mouse; 214 min in human)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

319.42

Formula

C19H17N3S

CAS No.
SMILES

C1(CCNC2=NC(C3=CNC4=C3C=CC=C4)=CS2)=CC=CC=C1

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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T2M-010
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HY-178324
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